Bismuth chelate as a contrast agent for X-ray computed tomography

Author:

Fu Ji-junORCID,Guo Jun-jie,Qin Ai-ping,Yu Xi-yong,Zhang Qiang,Lei Xue-ping,Huang Yu-gang,Chen Ming-yue,Li Jie-xia,Zhang Yu,Liu Jing-ping,Dang Yuan-ye,Wu Dan,Zhao Xiao-ya,Lin Zhong-xiao,Lin Yin-lei,Li Song-pei,Zhang Ling-yan

Abstract

Abstract Backgrounds Due to the unexpected side effects of the iodinated contrast agents, novel contrast agents for X-ray computed tomography (CT) imaging are urgently needed. Nanoparticles made by heavy metal elements are often employed, such as gold and bismuth. These nanoparticles have the advantages of long in vivo circulation time and tumor targeted ability. However, due to the long residence time in vivo, these nanoparticles may bring unexpected toxicity and, the preparation methods of these nanoparticles are complicated and time—consuming. Methods In this investigation, a small molecular bismuth chelate using diethylenetriaminepentaacetic acid (DPTA) as the chelating agent was proposed to be an ideal CT contrast agent. Results The preparation method is easy and cost—effective. Moreover, the bismuth agent show better CT imaging for kidney than iohexol in the aspect of improved CT values. Up to 500 µM, the bismuth agent show negligible toxicity to L02 cells and negligible hemolysis. And, the bismuth agent did not induce detectable morphology changes to the main organs of the mice after intravenously repeated administration at a high dose of 250 mg/kg. The pharmacokinetics of the bismuth agent follows the first—order elimination kinetics and, it has a short half—life time of 0.602 h. The rapid clearance from the body promised its excellent biocompatibility. Conclusions This bismuth agent may serve as a potential candidate for developing novel contrast agent for CT imaging in clinical applications.

Funder

National Natural Science Foundation of China

Natural Science Foundation of Guangdong Province

Science and Technology Program of Guangzhou

Traditional Chinese Medicine Program of Guangdong Province

the scientific research start-up fund for high-level talents of Foshan University, China

Publisher

Springer Science and Business Media LLC

Subject

Pharmaceutical Science,Applied Microbiology and Biotechnology,Biomedical Engineering,Molecular Medicine,Medicine (miscellaneous),Bioengineering

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